University of Illinois

University of California

The University of Texas System

Centre National De La Recherche Scientifique

Duke University

Memorial Sloan Kettering Cancer Center

International Minerals & Chemical Corp.

Stevens Institute of Technology

Universitéde Strasbourg

Centre National De La Recherche Scientifique-cnrs

John A Katzenellenbogen

Sung Hoon Kim

Benita Katzenellenbogen

Seema K Tiwari-Woodruff

Pierre H Chambon

Donald P McDonnell

Huimin Zhao

Martin J Jacobs

Daniel Metzger

Teresa A Martin

Julie A Pollock

Philip Shaul

John D Norris

Weiyi Toy

Alexander Parent

Lucia Wang

Sarat Chandarlapaty

Jillian Gunther

Abhishek Sharma

Zeynep Madak-Erdogan

Kathryn E Carlson

Shengjia Lin

Younghoon Kim

Noah Bindman

Melikhan Tanyeri

Charles M Schroeder, Iii

4-Hydroxyphenyl-2H-indazol-5-ol compounds are estrogen receptor beta ligands that have immunomodulatory properties and increase oligodendrocyte survival, differentiation, and remyelination. The compounds, compositions, and kits are useful in the treatment of multiple sclerosis and endometriosis.

Estrogen receptor beta ligands for the prevention and treatment of multiple sclerosis (MS) and other demyelinating, inflammatory and neurodegenerative diseases

Provided are compounds, or pharmaceutically acceptable salts thereof, which are useful for inhibiting FOXM1, inhibiting cancer growth, and/or treating cancer. In particular, these compounds and their corresponding quaternary ammonium salts may be used to treat various forms of breast cancer.

FOXM1 inhibitor compositions and methods of using the same

A genus of proteolysis-targeting chimeras (PROTACs)-type compounds/antiestrogens has now been found that act as selective estrogen receptor degraders (SERDs) and estrogen receptor antagonists by degrading and antagonizing ERa in breast cancer cells. The compounds are of the following genus: The compounds described herein exhibit anti-proliferative effects, and are potentially useful, alone or in combination with other therapies, for the treatment of breast cancer. In general, these compounds combine a tight binding ERa targeting ligand tethered to a recognition motif or degron. Once bound, the degron recruits destructive cellular components and the targeted receptor (i.e., ERa) is degraded (i.e., destroyed) or antagonized. 

Antiestrogen compounds

Provided are compounds of formulae provided herein. The compounds may include pathway-preferential estrogens (PaPEs) derivatives with tissue-selective activities. Also provided are pharmaceutical compositions comprising the compounds, as well as methods of treating a disease or condition including administering the compounds. The disease or condition may include postmenopausal symptoms, cardiovascular disease, stroke, vascular disease, bone disease, metabolic disease, arthritis, osteoporosis, obesity, vasomotor/hot flush, cognitive decline, cancer including breast cancer.

Compounds which activate estrogen receptors and compositions and methods of using the same

The present disclosure provides tetra-substituted cyclobutane inhibitors of Androgen Receptor Action, and methods of using such inhibitors, for the treatment of hormone-refractory cancers.

Tetra-aryl cyclobutane inhibitors of androgen receptor action for the treatment of hormone refractory cancer

The invention provides dendrimers, conjugates thereof, and methods of using dendrimer conjugates. In one embodiment, the invention provides novel polymeric dendrimers as a new class of fluorescent labels. The labels can include multiple fluorescent dye molecules conjugated to a single polymeric backbone or core, such as a dendrimer. The dendrimers can have regular or irregular branched polymeric network structures that allow for the chemical attachment of multiple dye molecules, multiple color dyes, and/or multiple functional groups, in a combinatorial fashion. The fluorescent dendritic nanoprobes (FDNs) thus provide a new class of fluorescent reporters for fluorescence microscopy and imaging.

Dye-conjugated dendrimers

The present invention relates to a method for tightly temporally controlling the biological activity of a protein of interest in a vertebrate, upon induction of the activity of a fusion protein comprising said protein of interest and an ERM polypeptide containing a mutated ligand binding domain of the human oestrogen receptor &#x3b1;, with a synthetic ligand that does not interfere with oestrogen signalling. In particular, the present invention concerns a method for generating tightly temporally-controlled targeted somatic mutations in a vertebrate, preferably a mouse, by inducing the activity of a fusion protein comprising a site-specific recombinase protein and an ERM polypeptide, with a synthetic ligand devoid of oestrogenic and anti-oestrogenic activities.

Method for controlling the biological activity of a protein in a vertebrate cell

Estriol is administered to ruminants in dosages from about 0.01-4.0 mg/ruminant/day to promote growth and increase feed utilization efficiency.

Estriol growth promotant

Aliphatic acids containing an isoprenoid 1,5-diene moiety are prepared in high yields by the selective gamma alkylation of .alpha.,.beta.-unsaturated acids with allylic electrophiles. The gamma-regioselectivity of the alkylation is controlled by the use of the dicopper(I) dienolates prepared from the .alpha.,.beta.-unsaturated acids. The method offers a particularly facile means for synthesizing isoprenoid 1,5-diene natural products such as farnesoic acid by alkylation of senecioic acid with geranyl bromide; geranoic acid by alkylation of senecioic acid with 3,3-dimethallyl bromide; and dl-lanceol by alkylation of tiglic acid with an allylic bromide derived from dl-limonene. Such products find use in the synthesis of insect pheremones, insect juvenile hormones, and components of perfumes.

Synthesis of isoprenoid 1,5-dienes

Growing community of inventors

Urbana, IL, United States of America

John A Katzenellenbogen